Liposomes are promising carriers for the encapsulation of drug molecules and subsequent delivery to the respiratory tract. The advantages of liposomes as carriers have been widely reported in literature, there are however associated disadvantages such as stability issues when suspended in aqueous media. This has been remedied partially by proliposome formulations (i.e. dry formulation of lipid with carbohydrate carrier). The aim of this work was to develop a novel solid dosage form of "proliposome tablets" (a precursor of liposomes), entrapping beclometasone dipropionate (BDP) as a model hydrophobic drug for the treatment or prophylaxis of asthma. 
A novel proliposome formulation method was developed in this study called the "Slurry" method, which is readily scalable to an industrial level. Soya Phosphatidylcholine (SPC) was utilised as the phospholipid component in combination cholesterol, in addition to four carbohydrate carriers (i.e. Lactose monohydrate (LMH), sucrose, sorbitol and D-mannitol), in three formulation ratios (i.e. 1:5, 1:10 and 1:15 w/w lipid to carrier) for the preparation of proliposome powders and tablets. Two dispersion media; deionised water (DW) or deuterium oxide (D2O) were used to generate liposomes from the formulated powders and tablets. Transmission Electron Microscopy studies confirmed that the generated liposomes from the proliposome formulations were multivesicular liposomes. In literature, the entrapment efficiency values in DW are recorded to be in excess of 80%. Using D2O, a novel separation method was developed, through which the entrapment efficiency of BDP in the generated liposomes was found to be in the range of 19.69 - 61.91%, showing great disparity in entrapment efficiency when compared to entrapment in DW. BDP entrapment efficiency was found in the following order of carriers used: Sorbitol > Sucrose > D-mannitol > LMH. 
D-mannitol and sorbitol-based powder formulations were assessed in terms of flowability via tapped density (17.81 + 4.46%) and angle of repose (25.62 + 1.08°), classifying sorbitol as possessing good to excellent flowability. Upon tableting of sorbitol and D-mannitol, formulations at lipid to carrier ratios of 1:10 and 1:15 w/w; were viably compressible into tablets. Furthermore, sorbitol-based tablets at a ratio of 1:15 w/w were observed to be the only carrier-based formulation, using the automated function of the Minipress tablet machine (20 + 2 tablets/minute with a compression force of 3.00 - 4.50 kN). The manufactured tablets were tested in accordance with British and US Pharmacopeial standards. Nebulization studies of formulated proliposome powders and tablets (Sorbitol and D-mannitol-based) were conducted to identify the most efficient formulation for pulmonary delivery. Tablets manufactured from sorbitol-based proliposome powders (1:15 w/w ratio) offered the shortest nebulization and sputtering times (24.18 + 0.16 and 2.42 + 0.54 minutes), with a high output rate (180.20 + 0.31 mg/minute). Liposome size for the 1:15 w/w lipid to carrier ratio, prior to nebulization, for sorbitol tablets was 5.85 + 0.86 µm. Moreover, this size was smaller than the liposomes found in the nebulizer reservoir i.e. (10.38 + 1.11 µm). Based on entrapment efficiency, tableting and nebulization studies, sorbitol-based proliposome formulations at the 1:15 w/w lipid to carrier ratio; a six-month stability study was carried out under various conditions (Room, Fridge and Hot temperature i.e. 22 + 1°C, 6 + 1°C and 40 + 1°C), and testing (size, charge, entrapment efficiency and a set of quality control tests) at monthly intervals. Liposome size increased dramatically from the control sample size (5.9 + 0.7 µm), to (9.19 + 0.81 µm) at 40°C on month six. The entrapment efficiency dropped significantly at 40°C decreasing from 57.43 + 9.12% (control tablets) to 32.56 + 5.47% at the sixth month of Hot temperature storage. This was posed to be due to degradation of the lipid under high temperature.
These research findings established sorbitol-based proliposome formulations (in a 1:15 w/w lipid to carrier ratio) to be the most appropriate for tableting on an industrial scale. Proliposome formulation and entrapment efficiency studies identified a novel method of liposome separation and proliposome manufacture. Nebulization and stability studies indicated that proliposome tablets are a viable option for pulmonary drug delivery eliciting high stability when sorbitol was used carbohydrate carrier in proliposome.

Nanotechnology in pulmonary drug delivery: Compressible proliposome formulations for nebulization

Study of the technological parameters of ultrasonic nebulisation

Handle everyday research tasks with reliable, citation-backed results

Your personal Research Agent to handle research tasks with citation-backed results

Popular Tasks used by Researchers

How can I help with your research?

Meet SciSpace

Get more enhanced response by uploading the PDFs you want me to reference.

No relevant PDFs in your library

SciSpace is the AI research assistant for academics. Run systematic literature reviews on 280M+ papers, and write papers with cited sources. Trusted by 1M+ students, PhDs & researchers.

SciSpace | AI for Research

Analyze PDFs

Code & Manuscripts

Funding & Grants

Literature & Patents

Medical & Clinical Data

Systematic Review

Visualize & Present

Web & Data

Build a Google Scholar-like website for your research.

Build a website

Create charts and images for your research

Create a Chart

Write a paper for submission to a journal

Draft a manuscript

Patent Search

Design eye-catching scientific posters in minutes.

Scientific Poster Generation

Systematic Literature Review

One task is running at the moment. Your messages will be shown right after.

Drag and drop or click here to browse

Loved by <highlight>1 million+</highlight> researchers

Extract a list of specific topics and their sources from unstructured text

Topics

Compare and analyze relevant papers that matches with your search

Papers

Get insights from PDFs and bookmarked papers from your library

My library

Recent searches

Try searching for:

Catch AI-generated content in scholarly and non-scholarly content

{ai} Detector

Ai Writer

Get PDF Summaries, highlighted text explanations 

Chat with PDF

Effortlessly create in-text citations and bibliographies in APA and 2,500 other formats

Citation generator

Get explanations, summaries, and answers on academic papers

Ease up your research workflow with {scispace}'s cohort of exciting AI tools

Elevate your academic writing skills and convey your ideas the way you want

Paraphraser

Explore our range of reading and writing tools

Your file is being prepared and should be ready in a few minutes. If it's a large file, it might take a bit longer. You can close this window, and we'll email you the file when it's done.

You have reached a maximum limit of <strong>{limit}</strong> columns in the table. Remove at least <strong>1</strong> column to add or create another one.

Study of the technological parameters of ultrasonic nebulisation

Chat with Paper

AI Agents for this Paper

Citations

Nanotechnology in pulmonary drug delivery: Compressible proliposome formulations for nebulization

References

Nanotechnology in pulmonary drug delivery: Compressible proliposome formulations for nebulization

Related Papers (2)

Assessment of Ultrasonic Nebulization

A review of ultrasonic nebulization.